Abstract: The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor ? (PPAR?) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.
Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
Type:
Grant
Filed:
February 1, 2003
Date of Patent:
December 27, 2005
Assignee:
The Regents of the University of California
Inventors:
Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
Abstract: Compounds of the general formula (I) wherein R1 represents halogen, R2 represent H or halogen, and R3 represents C3-8-cycloalkyl, C3-8-cycloalkenyl, or optionally substituted phenyl, pharmaceutical compositions containing such material, and methods of using such materials in the treatment of various diseases are disclosed and claimed.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
September 6, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Michael Härter, Michael Hahn, Claudia Hirth-Dietrich, Andreas Knorr, Elke Stahl, Johannes-Peter Stasch, Frank Wunder
Abstract: The invention relates to compounds of the general formula (I) wherein R1 represents H, halogen, or OCF3; R2 and R3 each represents H or halogen; R4 represents C1-6-alkyl, C3-8-cycloalkyl, CF3, OCF3, F, Cl, OMe, or optionally substituted phenyl; V represents O, CH2O, OCF2, or O—C1-6-alkyl-O; and W represents CH2 or CH2CH2. A process for making such compounds, pharmaceutical compositions containing them, and methods of treatment of various conditions using them are also disclosed and claimed.
Type:
Grant
Filed:
February 18, 2002
Date of Patent:
September 6, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Michael Härter, Michael Hahn, Claudia Hirth-Dietrich, Andreas Knorr, Elke Stahl, Johannes-Peter Stasch, Frank Wunder
Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive.
Type:
Grant
Filed:
January 3, 2003
Date of Patent:
May 10, 2005
Assignee:
Virbac SA
Inventors:
Ahmed El Hadri, Philippe Archimbault, Gérard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.
Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I):
New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.
Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
Type:
Grant
Filed:
October 1, 2001
Date of Patent:
August 17, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
Abstract: A novel means for DNA compaction is provided.
The object is accomplished by providing a fullerene derivative having 1 to 4 nitrogen-containing hydrophilic side chain(s) or its salt for DNA compaction.
DNA compaction can be achieved effectively, and application to gene therapy is also expected.
Abstract: New carbocyclic compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease, other neurodegenerative disorders, such as Parkinson's disease and Huntington's disease, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
Type:
Application
Filed:
October 20, 2003
Publication date:
July 15, 2004
Inventors:
Allan S. Wagman, Sharadha Subramanian, John M. Nuss
Abstract: A method for preparing a solid support material for carrying out a chemical reaction, said method comprising the following steps:
(i) reacting an amino functionalised solid material with a carboxylic acid having at least two similarly protected amino groups to form amide bonds between them,
(ii) removing protecting groups in a single step,
(iii) optionally repeating steps (i) and (ii) one or more times using the product of the preceding step as the amino functionalised solid material, and
(iv) connecting a linkage agent to at least some of the free NH2 groups of the product.
The method increases the loading capacity of the solid support material. It is particularly useful in connection with peptide synthesis.
Type:
Grant
Filed:
March 26, 2002
Date of Patent:
June 15, 2004
Assignee:
Avecia Limited
Inventors:
Craig Stephen Harris, Donald Alfred Wellings, Francis Joseph Montgomery, Richard John Brown
Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
Abstract: O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1)
[wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.
Type:
Grant
Filed:
March 18, 2002
Date of Patent:
March 16, 2004
Assignee:
Kyorin Pharmaceutical Co., Ltd.
Inventors:
Hiroya Satoh, Masakatsu Komuro, Koji Murakami, Katsuya Awano
Abstract: The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.
Type:
Application
Filed:
August 18, 2003
Publication date:
February 19, 2004
Inventors:
Pascal Druzgala, Peter G. Milner, Jurg Pfister, Xiaoming Zhang
Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1)
wherein
R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
Type:
Grant
Filed:
April 6, 2001
Date of Patent:
January 13, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
Abstract: An organic compound useful for detecting the total quantity of isocyanate in an environmental sample is provided. The compound is 9-anthrcenylmethyl-1-piperazinecarboxylate (PAC), an isocyanate derivatizing agent. A process for producing PAC and methods for detecting a particular isocyanate monomer or the total isocyanate in environmental samples using PAC & related isocyanate derivatizing agents are also provided.
Type:
Grant
Filed:
November 10, 2000
Date of Patent:
December 2, 2003
Assignee:
The United States of America as represented by the Department
of Health and Human Services
Abstract: The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.
Abstract:
or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
Type:
Grant
Filed:
August 22, 2001
Date of Patent:
September 30, 2003
Assignee:
Abbott Laboratories
Inventors:
Gang Liu, Yihong Li, David A. Janowick, Zhonghua Pei
Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive. These derivatives comply with the general formula (I) in which R2 represents one of the following groups: —CH2—, —CH2—CH2, —CH(CH3)—CH2—, —C(CH3)═CH—, —C(CH3)2—CH2— or a bond; Q represents: (i) a phenyl radical 3,4-disubstituted alkylene dioxy determining with the phenyl radical, a non-substituted benzodioxane unit, a non-substituted benzodioxol unit, or a 2-substituted benzodioxol unit, (ii) a phenyl radical 3 and/or 4-substituted, by a O—(CH2)x—COOR5 group, (iii) a condensed polycyclic hydrocarbon comprising at least two condensed cycles, (iv) a cyclic hydrocarbon system, optionally cross-linked, and constituting a cycloalkane comprising 1, 2 or 3 cycles.
Type:
Application
Filed:
January 3, 2003
Publication date:
August 21, 2003
Applicant:
VIRBAC SA
Inventors:
Philippe Archimbault, Gerard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR).
Type:
Application
Filed:
October 16, 2002
Publication date:
June 12, 2003
Inventors:
Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, John Patrick Mogensen
Abstract: The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
Type:
Application
Filed:
April 16, 2002
Publication date:
April 24, 2003
Applicant:
Pfizer Inc.
Inventors:
David Clive Blakemore, Justin Stephen Bryans, Sophie Caroline Williams
Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.
Type:
Application
Filed:
October 9, 2001
Publication date:
February 13, 2003
Inventors:
Klaus Urbahns, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Berthold Hinzen, Elke Dittrich-Wengenroth, Hilmar Bischoff, Claudia Hirth-Dietrich, Klemens Lustig
Abstract: The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor &agr; (PPAR&agr;), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride).
It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1),
their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.
Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
Type:
Grant
Filed:
November 16, 2001
Date of Patent:
January 7, 2003
Assignee:
Eli Lilly and Company
Inventors:
Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I:
where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Type:
Grant
Filed:
August 28, 2000
Date of Patent:
December 17, 2002
Assignee:
Cytovia, Inc.
Inventors:
Yan Wang, Sui Xiong Cai, Eckard Weber, Gordon B. Mills, Douglas R. Green, Lufeng Guan
Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
Type:
Application
Filed:
November 16, 2001
Publication date:
December 12, 2002
Inventors:
Carsten Behrens, Jesper Lau, Peter Madsen
Abstract: Amides of the general formula I
and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings:
R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and
R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and
X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic]
R1—X [sic] together are also
and
R3 [sic] is hydrogen and CO—NR6R7 [sic],
R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched an
Abstract: The invention herein is directed to a process for the preparation of chiral &bgr;-amino acids and esters of the formula
wherein X and Y are the same or different halo groups, R2 is H or lower alkyl and isomers and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
March 2, 1999
Date of Patent:
July 2, 2002
Assignee:
G. D. Searle
Inventors:
Pierre-Jean Colson, Alok K. Awasthi, Srinivasan R. Nagarajan
Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formulae I-VII of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
Type:
Grant
Filed:
March 10, 1999
Date of Patent:
June 25, 2002
Inventors:
Scott D. Larsen, Paul D. May, John E. Bleasdale, Charlotta Liljebris, Heinrich Josef Schostarez, Tjeerd Barf, Marianne Nilsson
Abstract: Novel aminoethylphenoxyacetic acid derivatives represented by the general formula:
(wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom or a halogen atom; the carbon atom marked with (R) represents a carbon atom in (R) configuration; and the carbon atom marked with (S) represents a carbon atom in (S) configuration) and pharmaceutically acceptable salts thereof, which have stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and are useful as agents for relieving pain and promoting the removal of calculi in urolithiasis.
Abstract: A method for enhancing the purity of a desired compound comprising:
Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents;
Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and
Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.
Abstract: Ureins are obtained by reaction, in basic medium, between an N&ohgr;-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.
Type:
Application
Filed:
September 4, 2001
Publication date:
May 16, 2002
Inventors:
Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
Abstract: The present invention relates to a crystalline polymorph of 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl]amino]ethyl]phenoxy]acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;±0.1°) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0° in powder X-ray diffraction pattern, which has potent &bgr;2- and &bgr;3-adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-amino]ethyl]phenoxy]acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40° C. and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40° C. to reflux temperature for 30 minutes to several hours.
Abstract: The invention relates to novel processes for preparing differentially protected lysine derivatives via a novel p-anisaldehyde Schiff base intermediate and the intermediate prepared therein.
Abstract: The invention concerns aryloxypropanolamnine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive. These derivatives comply with the general formula (I) in which R2 represents one of the following groups: —CH2—, —CH2—CH2, —CH(CH3)—CH2—C(CH3)—CH—, —C(CH3)2—CH2— or a bond; Q represents: (i) a phenyl radical 3,4-substituted alkylene dioxy determining with the phenyl radical, a non-substituted benaodioxane unit, a non-substituted benzodioxol unit, or a 2-substituted benzodioxol unit, (ii) a phenyl radical 3 and/or 4-substituted, by a O—(CH2)x—COOR5 group, (iii) a condensed polycyclic hydrocarbon comprising at least two condensed cycles, (iv) a cyclic hydrocarbon system, optionally cross-linked, and constituting a cycloalkane comprising 1, 2 or 3 cycles.
Type:
Application
Filed:
August 23, 2001
Publication date:
February 14, 2002
Applicant:
VIRBAC SA
Inventors:
Archimbault Philippe, Leclerc Gerard, Strosberg Arthur Donny, Pietri-Rouxel France
Abstract: The invention includes synthetic immunochemical haptens for the generation of antibodies, the antibodies, and the medical treatment applications for using the antibodies. The antibodies are designed to recognize the common molecular features of d-methamphetamine-like abused stimulants, and will have insignificant cross-reactivity with endogenous substrates (e.g. dopamine) or over-the-counter medications (e.g. 1-methamphetamine, pseudoephedrine, phenylpropanolamine and ephedrine). These monoclonal antibodies and their antigen binding fragments are useful in treatment plans for recovering addicts, in emergency room settings for rapidly reversing a drug overdose, in protection of fetuses or fetus from drug-abusing pregnant mothers or in a psychiatric setting to reduce the exacerbation of psychotic disorders caused by stimulant drugs.
Type:
Application
Filed:
April 20, 2001
Publication date:
December 13, 2001
Inventors:
Samuel M. Owens, Frank Ivy Carroll, Philip Abraham
Abstract: The invention relates to compound of formula (I):
A—G1—Cy—G2—Cy′—G3—B (I)
wherein:
A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3,
B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3,
G1 and G3 represent an optionally substituted alkylene chain,
Cy and Cy′, which are different, represent a ring structure
or
G2 represents a chain
and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
Type:
Grant
Filed:
May 18, 2000
Date of Patent:
October 30, 2001
Assignee:
Adir et Compagnie
Inventors:
Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois